GSK6853, a Chemical Probe for Inhibition of the BRPF1 Bromodomain

Paul Bamborough; Heather Barnett; Isabelle Becher; Mark J. Bird; Chun‐wa Chung; Peter D. Craggs; Emmanuel H. Demont; Hawa Diallo; David J. Fallon; Laurie Gordon; Paola Grandi; Clare I. Hobbs; Edward Hooper‐Greenhill; Emma J. Jones; Robert P. Law; Armelle Le Gall; David Lugo; Anne‐Marie Michon; Darren J. Mitchell; Rab K. Prinjha; Robert J. Sheppard; Allan J. B. Watson; Robert J. Watson

doi:10.1021/acsmedchemlett.6b00092

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Abstract

The BRPF (Bromodomain and PHD Finger-containing) protein family are important scaffolding proteins for assembly of MYST histone acetyltransferase complexes. A selective benzimidazolone BRPF1 inhibitor showing micromolar activity in a cellular target engagement assay was recently described. Herein, we report the optimization of this series leading to the identification of a superior BRPF1 inhibitor suitable for in vivo studies.

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Bamborough et al. (2016) studied this question.

synapsesocial.com/papers/6aaf7ee04687f6dd6a76f0ea https://doi.org/10.1021/acsmedchemlett.6b00092

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GSK6853, a Chemical Probe for Inhibition of the BRPF1 Bromodomain

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GSK6853, a Chemical Probe for Inhibition of the BRPF1 Bromodomain

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